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Toward Overcoming Staphylococcus aureus Aminoglycoside Resistance Mechanisms with a Functionally Designed Neomycin Analogue.
Hanessian, Stephen; Giguère, Alexandre; Grzyb, Justyna; Maianti, Juan Pablo; Saavedra, Oscar M; Aggen, James B; Linsell, Martin S; Goldblum, Adam A; Hildebrandt, Darin J; Kane, Timothy R; Dozzo, Paola; Gliedt, Micah J; Matias, Rowena D; Feeney, Lee Ann; Armstrong, Eliana S.
Affiliation
  • Hanessian S; Department of Chemistry, Université de Montréal , C.P. 6128, Succ. Centre-Ville, Montréal, Quebec H3C 3J7, Canada.
  • Giguère A; Department of Chemistry, Université de Montréal , C.P. 6128, Succ. Centre-Ville, Montréal, Quebec H3C 3J7, Canada.
  • Grzyb J; Department of Chemistry, Université de Montréal , C.P. 6128, Succ. Centre-Ville, Montréal, Quebec H3C 3J7, Canada.
  • Maianti JP; Department of Chemistry, Université de Montréal , C.P. 6128, Succ. Centre-Ville, Montréal, Quebec H3C 3J7, Canada.
  • Saavedra OM; Department of Chemistry, Université de Montréal , C.P. 6128, Succ. Centre-Ville, Montréal, Quebec H3C 3J7, Canada.
  • Aggen JB; Achaogen Inc. , 7000 Shoreline Court, Suite 371, South San Francisco, California 94080, United States.
  • Linsell MS; Achaogen Inc. , 7000 Shoreline Court, Suite 371, South San Francisco, California 94080, United States.
  • Goldblum AA; Achaogen Inc. , 7000 Shoreline Court, Suite 371, South San Francisco, California 94080, United States.
  • Hildebrandt DJ; Achaogen Inc. , 7000 Shoreline Court, Suite 371, South San Francisco, California 94080, United States.
  • Kane TR; Achaogen Inc. , 7000 Shoreline Court, Suite 371, South San Francisco, California 94080, United States.
  • Dozzo P; Achaogen Inc. , 7000 Shoreline Court, Suite 371, South San Francisco, California 94080, United States.
  • Gliedt MJ; Achaogen Inc. , 7000 Shoreline Court, Suite 371, South San Francisco, California 94080, United States.
  • Matias RD; Achaogen Inc. , 7000 Shoreline Court, Suite 371, South San Francisco, California 94080, United States.
  • Feeney LA; Achaogen Inc. , 7000 Shoreline Court, Suite 371, South San Francisco, California 94080, United States.
  • Armstrong ES; Achaogen Inc. , 7000 Shoreline Court, Suite 371, South San Francisco, California 94080, United States.
ACS Med Chem Lett ; 2(12): 924-8, 2011 Dec 08.
Article in En | MEDLINE | ID: mdl-24900282
ABSTRACT
Deoxygenation of the diol groups in rings A and D of neomycin in combination with the introduction of an N1-(l)-HABA group in the 2-deoxystreptamine subunit (ring B) leads to a novel and potent antibiotic (1) with activity against strains of S. aureus carrying known aminoglycoside resistance determinants, as well as against an extended panel of Methicillin-resistant S. aureus isolates (n = 50). Antibiotic 1 displayed >64 fold improvement in MIC50 and MIC90 against this MRSA collection when compared to the clinically relevant aminoglycosides amikacin and gentamicin. The synthesis was achieved in six steps and 15% overall yield.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Language: En Journal: ACS Med Chem Lett Year: 2011 Document type: Article Affiliation country: Canada
Fulltext
Add to My VHL
Print
XML
PubMed Links
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Full text: 1 Collection: 01-internacional Database: MEDLINE Language: En Journal: ACS Med Chem Lett Year: 2011 Document type: Article Affiliation country: Canada